Polygonum cuspidatum has been proved to have the pharmacological effect of normalizing the gallbladder to treat jaundice, and has been used in clinical treatment of cholestatic liver disease and icteric hepatitis. Therefore, it is important to explore its pharmacological mechanism of normalizing the gallbladder to treat jaundice to expand its clinical application and carry out further research on Polygonum cuspidatum. At present, there have been some studies on the pharmacological mechanism of Polygonum cuspidatum, mainly from the two metabolic pathways of bile acid metabolism and bilirubin metabolism as entry points for in-depth research. In this paper, based on the research of relevant literature, starting from the active components and compound preparations of Polygonum cuspidatum, it is found that the current research mainly focuses on the enzymes that affect the homeostasis of bile acid and bilirubin in the body or the transporters regulated by the farnesoid X receptor. In addition, there are also studies that found that inflammation and oxidative stress are also related to cholestasis. Therefore, the research progress of the pharmacological action mechanism of Polygonum cuspidatum for normalizing the gallbladder to treat jaundice is reviewed from these perspectives. It is expected to lay a foundation for further study of Polygonum cuspidatum.

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